823817-56-7Relevant articles and documents
Two methods for the preparation of sitagliptin phosphate: Via chemical resolution and asymmetric hydrogenation
Ye, Fei,Zhang, Zhifeng,Zhao, Wenxia,Ding, Jianhai,Wang, Yali,Dang, Xueyan
, p. 4805 - 4809 (2021/02/03)
Two effective processes have been developed for the preparation of sitagliptin phosphate. The approach of chemical resolution obtained R-sitagliptin in five steps from commercially available starting materials using the inexpensive NaBH4 to reduce the enamine and then using (-)-di-p-toluoyl-l-tartaric acid to resolve racemates in 11% yield overall. The route successfully avoids the use of expensive noble metal as catalysts compared with traditional synthesis methods, resulting in greatly reduced costs and simplified synthetic routes. Other alternative asymmetric hydrogenation of β-ketomide routes for the synthesis of sitagliptin were found, two of the intermediates were synthesized for the first time. This journal is
A process for the conversion of isomer
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Paragraph 0053; 0054, (2016/11/17)
The invention relates to a method for recycling an isomer such as sitagliptin and belongs to the technical field of pharmacy. The isomer and mercaptan are transformed into a racemate under the action of a free radical initiator, and then a compound needin
A NOVEL SYNTHETIC APPROACH TO ?-AMINOBUTYRYL SUBSTITUTED COMPOUNDS
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, (2011/12/14)
The present invention relates to process to prepare β-aminobutyryl compounds of formula (I), wherein Q is N, CH, C-CF3 or C-phenyl, preferably N, and R10 is H, C1-C4-alkyl or fluorinated C1C2-alkyl, preferably trifluoromethyl, and wherein X is halogen selected from fluoro, chloro, or bromo, preferably fluoro, same or different, and n is 1-4.